EP 3871667 A4 20220817 - PPAR DELTA ACTIVATOR
Title (en)
PPAR DELTA ACTIVATOR
Title (de)
PPAR-DELTA-AKTIVATOR
Title (fr)
ACTIVATEUR DE PPAR?
Publication
Application
Priority
- JP 2018199523 A 20181023
- JP 2019041563 W 20191023
Abstract (en)
[origin: EP3871667A1] The present invention provides a PPARδ activator containing a novel PPARδ agonist (peroxisome proliferator-activated receptor δ) as an active ingredient, and an exercise tolerance-improving agent containing the same as an active ingredient. The present invention is a PPARδ activator containing a guanidine derivative or a biguanidine derivative as an active ingredient, wherein the PPARδ activator activates transcriptional activity of PPARδ, and the guanidine derivative and the biguanidine deravative are capable of fitting within a PPARδ ligand binding pocket in a state where a guanidino group or a biguanidino group forms a hydrogen bond with amino acid residues corresponding to each of the 413th histidine, 287th histidine, 253rd threonine and the 437th tyrosine of human PPARδ, among amino acid residues constituting an interior surface of the ligand binding pocket; and is an exercise tolerance-improving agent containing the PPARδ activator as an active ingredient.
IPC 8 full level
C07D 277/26 (2006.01); A61K 31/155 (2006.01); A61K 31/426 (2006.01); A61P 3/00 (2006.01); A61P 43/00 (2006.01); C07C 279/04 (2006.01)
CPC (source: EP US)
A61K 31/155 (2013.01 - EP US); A61K 31/426 (2013.01 - EP US); A61P 3/00 (2017.12 - EP); A61P 43/00 (2017.12 - EP US); C07C 279/08 (2013.01 - EP); C07D 277/26 (2013.01 - EP); C07K 14/70567 (2013.01 - EP); C07C 2601/14 (2017.04 - EP)
Citation (search report)
- [A] WO 0100603 A1 20010104 - GLAXO GROUP LTD [GB], et al
- [A] WO 2008083330 A2 20080710 - SALK INST FOR BIOLOGICAL STUDI [US], et al
- [A] WU CHYUAN-CHUAN ET AL: "Structural basis for specific ligation of the peroxisome proliferator-activated receptor [delta]", PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCE PNAS, vol. 114, no. 13, 20 March 2017 (2017-03-20), pages E2563 - E2570, XP055938898, Retrieved from the Internet <URL:https://www.pnas.org/doi/pdf/10.1073/pnas.1621513114> DOI: 10.1073/pnas.1621513114
- See references of WO 2020085393A1
Designated contracting state (EPC)
AL AT BE BG CH CY CZ DE DK EE ES FI FR GB GR HR HU IE IS IT LI LT LU LV MC MK MT NL NO PL PT RO RS SE SI SK SM TR
DOCDB simple family (publication)
EP 3871667 A1 20210901; EP 3871667 A4 20220817; CN 112912069 A 20210604; JP 2023165025 A 20231114; JP 7397491 B2 20231213; JP WO2020085393 A1 20210909; SG 11202103984W A 20210528; US 2022031666 A1 20220203; WO 2020085393 A1 20200430
DOCDB simple family (application)
EP 19875990 A 20191023; CN 201980069412 A 20191023; JP 2019041563 W 20191023; JP 2020553434 A 20191023; JP 2023149458 A 20230914; SG 11202103984W A 20191023; US 201917286904 A 20191023